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US 2017/0291892 A1Published application
Substituted oxopyridine derivatives
AssigneeBayer Pharma Aktiengesellschaft
InventorsSusanne RÖHRIG, Eloisa JIMENEZ-NUNEZ, Karl-Heinz SCHLEMMER, Adrian TERSTEEGEN, Henrik TELLER, Alexander HILLISCH, Stefan HEITMEIER, Martina Victoria SCHMIDT, Jens ACKERSTAFF, Jan STAMPFUß
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Abstract
The invention relates to substituted oxopyridine derivatives and to processes for preparation thereof, and also to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.
Claims14
Compound of the formula
- in which
- R1 is a group of the formula
- steht,
- where * is the attachment point to the oxopyridine ring,
- R6 is bromine, chlorine, fluorine, methyl, difluoromethyl, trifluoromethyl, methoxy, difluoromethoxy, trifluoromethoxy or methylamino,
- R7 is bromine, chlorine, fluorine, cyano, nitro, hydroxyl, methyl, difluoronnethyl, trifluoromethyl, methoxy, ethoxy, difluoronnethoxy, trifluoromethoxy, ethynyl, 3,3,3-trifluoroprop-1-yn-1-yl or cyclopropyl,
- R8 is hydrogen, chlorine or fluorine,
- R2 is hydrogen, bromine, chlorine, fluorine, cyano, C1-C3-alkyl, difluoromethyl, trifluoromethyl, 1,1-difluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, C1-C3-alkoxy, difluoromethoxy, trifluoromethoxy, 1,1-difluoroethoxy, 2,2-difluoroethoxy, 2,2,2-trifluoroethoxy, methylcarbonyl or cyclopropyl,
- R3 is hydrogen, C1-C5-alkyl, C1-C4-alkoxy, difluoromethyl, trifluoromethyl, 1,1-difluoroethyl, 1,1,2,2,2-pentadeuteroethyl, 3,3,3-trifluoro-2-hydroxyprop-1-yl, 3,3,3-trifluoro-2-methoxyprop-1-yl, 3,3,3-trifluoro-2-ethoxyprop-1-yl, prop-2-yn-1-yl, cyclopropyloxy or cyclobutyloxy,
- where alkyl may be substituted by a substituent selected from the group consisting of fluorine, cyano, hydroxyl, difluoromethyl, trifluoromethyl, methoxy, ethoxy, difluoromethoxy, trifluoromethoxy, C3-C6-cycloalkyl, 4- to 6-membered oxoheterocyclyl, 1,4-dioxanyl, oxazolyl, pyrazolyl, oxadiazolyl, dihydrooxazolyl, phenyl and pyridyl,
- in which cycloalkyl may be substituted by 1 to 2 substituents selected independently from the group consisting of fluorine, hydroxyl, methyl, ethyl, methoxy, ethoxy, difluoromethyl, trifluoromethyl, difluoromethoxy and trifluoromethoxy,
- and
- in which oxoheterocyclyl may be substituted by 1 to 2 substituents selected independently from the group consisting of oxo, fluorine, methyl, ethyl, difluoromethyl and trifluoromethyl,
- and
- in which oxazolyl, pyrazolyl and oxadiazolyl may be substituted by 1 to 2 substituents selected independently from the group consisting of methyl and ethyl,
- R4 is hydrogen,
- R5 is a group of the formula
- where # is the attachment point to the nitrogen atom,
- R12 is hydrogen or fluorine,
- R13 is hydroxyl or —NHR14,
- in which
- R14 is hydrogen or C1-C4-alkyl,
- or one of the salts thereof, solvates thereof or solvates of the salts thereof.
20 more elements
Dependencies are inferred from the claim text.